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OXYBUTYNIN HYDROCHLORIDE TABLETS 2.5 MG

Active substance(s): OXYBUTYNIN CHLORIDE / OXYBUTYNIN CHLORIDE / OXYBUTYNIN CHLORIDE

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SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Oxybutynin Hydrochloride Tablets 2.5mg.

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Oxybutynin Hydrochloride 2.5mg.
For excipients, see 6.1

3.

PHARMACEUTICAL FORM
Tablet.
Blue, biconvex, uncoated capsule-shaped tablets, marked OB scoreline 2.5 on
one side and plain on the reverse

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Adults: Urinary incontinence, urgency and frequency in unstable bladder
conditions due to idiopathic detrusor instability (motor urge incontinence) or
neurogenic bladder disorders (detrusor hyperreflexia) in conditions such as
multiple sclerosis and spinabifida.

Paediatric population
Oxybutynin hydrochloride is indicated in children over 5 years of age for:
• Urinary incontinence, urgency and frequency in unstable bladder
conditions due to idiopathic overactive bladder or neurogenic bladder
disorders (detrusor overactivity)
• Nocturnal enuresis associated with detrusor overactivity, in
conjunction with non-drug therapy, when other treatment has failed
4.2

Posology and method of administration
Adults

The usual initial dose is 5mg two or three times a day. This dose may be increased to
a maximum dose of 5mg four times a day to obtain a clinical response provided that
the side effects are well-tolerated.
Elderly (including frail elderly)
A lower dose is recommended because the elimination half-life is increased in the
elderly. A dose of 2.5mg twice a day is likely to be adequate, particularly if
the
patient is frail. This dose may be increased if necessary to 5mg twice a day
provided that the side effects are well tolerated.
Children (under 5 years of age)
Not recommended
Children (over 5 years of age)
Neurogenic bladder instability: The usual dose is 2.5mg twice a day. This dose
may be increased, if necessary, to 5mg two or three times daily provided that the side
effects are well-tolerated.
Nocturnal enuresis: The usual dose is 2.5mg twice a day. This dose may be
increased, if necessary, to 5mg two or three times daily provided that the side effects
are well-tolerated. The last dose should be given before bedtime.

4.3

Contraindications

Oxybutynin hydrochloride tablets are contraindicated in patients with:
Hypersensitivity to oxybutynin or any of the excipients.
Myasthenia Gravis
Narrow-angle glaucoma or shallow anterior chamber.
Gastrointestinal obstruction including paralytic ileus and intestinal atony.
Toxic megacolon, severe ulcerative colitis.
Patients with bladder flow obstruction where urinary retention may be precipitated.
Porphyria

4.4

Special warnings and precautions for use
Oxybutynin hydrochloride tablets should be used with caution in the frail elderly and
children who may be more sensitive to the effects of the product and in patients with
autonomic neuropathy (such as those with Parkinson’s disease), severe
gastrointestinal motility disorders, hepatic or renal impairment.

Anticholinergics should be used with caution in elderly patients due to the risk of
cognitive impairment.
Gastrointestinal disorders: Anticholinergic medicinal products may decrease
gastrointestinal motility and should be used with caution in patients with
gastrointestinal obstructive disorders, intestinal atony and ulcerative colitis.
Oxybutynin may aggravate tachycardia (and thus be cautious in case of
hyperthyroidism, congestive heart failure, cardiac arrhythmia, coronary heart disease,
hypertension), cognitive disorders and symptoms of prostatic hypertrophy.
Anticholinergic CNS effects (e.g. hallucinations, agitation, confusion, somnolence)
have been reported; monitoring recommended especially in first few months after
initiating therapy or increasing the dose; consider discontinuing therapy or reducing
the dose if anticholinergic CNS effects develop.
Since oxybutynin can cause narrow-angle glaucoma, patients should be advised to
contact a physician immediately if they are aware of a sudden loss of visual acuity or
ocular pain.
Oxybutynin may reduce salivary secretions which could result in dental caries,
parodontosis or oral candidiasis.
Anticholinergic medicinal products should be used with caution in patients who have
hiatus hernia/gastro-oesophageal reflux and/or who are concurrently taking medicinal
products (such as bisphosphonates) that can cause or exacerbate oesophagitis.
When oxybutynin is used in high environmental temperatures, this can cause heat
prostration due to decreased sweating.
Patients with rare hereditary problems of galactose intolerance, the LAPP lactase
deficiency or glucose-galactose malabsorption should not take this medicine.
Paediatric population:
The use of oxybutynin in children under 5 years of age is not recommended; it has not
been established whether oxybutynin can be safely used in this age group.
There is limited evidence supporting the use of Oxybutynin in children with
monosymptomatic nocturnal enuresis (not related to detrusor overactivity).
In children over 5 years of age, Oxybutynin hydrochloride should be used with
caution as they may be more sensitive to the effects of the product, particularly the
CNS and psychiatric adverse reactions.
4.5

Interaction with other medicinal products and other forms of interaction
Care should be taken if other anticholinergic agents are administered together with
oxybutynin, as potentiation of anticholinergic effects may occur.
The anticholinergic activity of oxybutynin is increased by concurrent use of other
anticholinergics or medicinal products with anticholinergic activity, such as
amantadine and other anticholinergic antiparkinsonian medicinal products (e.g.
biperiden, levodopa), antihistamines, antipsychotics (e.g. phenothiazines,
butyrophenones, clozapine), quinidine, digitalis, tricyclic antidepressants, atropine
and related compounds like atropinic antispasmodics and dipyridamole.

By reducing gastric motility, oxybutynin may affect the absorption of other drugs.
Oxybutynin is metabolised by cytochrome P 450 isoenzyme CYP 3A4. Concomitant
administration with a CYP3A4 inhibitor can inhibit oxybutynin metabolism and
increase oxybutynin exposure. Oxybutynin may antagonise prokinetic therapies.
Concomitant use with cholinesterase inhibitors may result in reduced cholinesterase
inhibitor efficacy.
Patients should be informed that alcohol may enhance the drowsiness caused by
anticholinergic agents such as oxybutynin (see section 4.7).
4.6

Pregnancy and lactation
Pregnancy:
There are no adequate data from the use of oxybutynin pregnant women.
Studies in animals have shown reproductive toxicity (see section 5.3).
The potential risk for humans is unknown. Oxybutynin should not be used in
pregnancy unless clearly necessary.
Lactation:
Oxybutynin is excreted in breast milk.
Oxybutynin should not be used during breast-feeding.

4.7

Effects on ability to drive and use machines
Oxybutynin hydrochloride tablets can cause drowsiness or blurred vision and
patients should be cautioned as to potential effects on the ability to drive,
operate machinery or perform hazardous work.

4.8

Undesirable effects

Very
Common
1/10

Common

Uncommon Rare

1/100 to
<1/10

1/1,000 to 1/10,000
to
<1/100
<1/1000

Not Known*

Infections and
infestations

urinary tract
infection

Immune
System
Disorders

hypersensitivity

Psychiatric

confusional

anxiety,

hallucinations,
nightmares
paranoia,
agitation,
cognitive
disorders in
elderly,
symptoms of
depression,
Dependence to
oxybutynin (in
patients with
history of drug
or substance
abuse)

state

disorders

Nervous System somnolence,
headache,
Disorders
dizziness,

Eye disorders

vision
blurred

Cognitive
disorders,
convulsions,
drowsiness,
disorientation
Angle closure
glaucoma,
mydriasis, ocular
hypertension

dry eyes

arrhythmia
tachycardia

Cardiac
disorders
Vascular
disorders

flushing
which may
be more
marked in
children

Gastrointestinal dry mouth, Diarrhea,
nausea,
vomiting
Disorders
constipation

anorexia,
dysphagia,
abdominal
discomfort,
decreased
appetite

gastroesophageal
reflux disease,
Pseudoobstruction in
patients at risk
(elderly or
patients with
constipation and
treated
with other drugs
that decrease
intestinal
motility)

Skin and
subcutaneous
tissue disorders

Angioedema,
rash, urticaria,
hypohidrosis,
photosensitivity

dry skin

Renal and
urinary
disorders

urinary
retention,

Injury,
poisoning and
procedural
complications

difficulty in
micturition
Heat stroke

*Cannot be estimated from the available clinical data.

Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is
important. It allows continued monitoring of the benefit/risk balance of the medicinal
product.
Healthcare professionals are asked to report any suspected adverse reactions via
Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.
4.9

Overdose
The symptoms of overdosage with oxybutynin progress from an intensification of the
usual side effects of CNS disturbances (from restlessness and excitement to psychotic
behaviour), circulatory changes (flushing, fall in blood pressure, circulatory failure
etc), respiratory failure, paralysis and coma.
Measures to be taken are:
1. Immediate gastric lavage
2. Physostigmine by slow intravenous injection
Adults: 0.5 to 2.0 mg of physostigmine by slow intravenous administration. Repeat
after 5 minutes, if necessary up to a maximum total dose of 5mg
Children: 30 micrograms/kg of physostigmine by slow intravenous administration.
Repeat after 5 minutes, if necessary up to a maximum total dose of 2mg.
Fever should be treated symptomatically with tepid sponging or ice packs.
In pronounced restlessness or excitation, diazepam 10mg may be given by
intravenous injection, tachycardia may be treated by intravenous injection of
propranolol and urinary retention can be managed by bladder catheterisation.
In the event of progression of the curare- like effect to the paralysis of the respiratory
muscles, mechanical ventilation will be required.

5.

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties

Urinary antispasmodics G04B D04
Oxybutynin has a direct antispasmodic effect on the smooth muscle of the
bladder
detrusor.
Oxybutynin also inhibits the effects of acetylcholine on smooth muscle by
blocking muscarinic receptors. Pharmacological models have established
differences in affinity for subtypes of muscarinic receptors.
The pharmacodynamic properties of oxybutynin result in relaxation of the
bladder detrusor muscle. Patients with unstable bladder experience increased
bladder volume and a decreased incidence of spontaneous contractions of the
detrusor muscle.

5.2

Pharmacokinetic properties
Following oral administration, oxybutynin is rapidly absorbed from the
gastrointestinal tract (tmax 0.5-1.4hours).
Studies have established a cmax after a 5-10mg dose in young healthy patients of
8-12ng/ml. Larger inter-individual variations in plasma concentrations are seen.
Oxybutynin is subject to extensive first pass metabolism, resulting in an
absolute systemic availability of 6.2%.
The major metabolite produced is desethyloxybutynin. Several other
metabolites are produced, including phenylcyclohexylglycolic acid.
Urinary excretion has been established as less than 0.02% of an administered
dose.
Oxybutynin is 83-85% plasma albumin bound.
Oxybutynin is eliminated biexponentially. Mean elimination half life is 2 hours.
Repeated administration results in little accumulation.

5.3

Preclinical safety data
Oxybutynin hydrochloride has been shown to have low acute toxicity when
administered orally to either mice, rats or dogs. In a repeat dosing experiment of
6 months duration in rats, daily oral doses of 63mg/kg or more were associated
with decreases in food consumption and body weight gain and with minor
pathological changes in the liver and kidneys. At daily oral doses of 6mg/kg
administered for 6 months, dogs exhibited transient anorexia, tremors and
nervousness but these effects were not associated with microscopic signs of
tissue damage.

There is no evidence from preclinical studies to suggest either mutagenic or
carcinogenic activity for oxybutynin.
Reproduction tests indicate no adverse effects on fertility or reproductive
performance in rats given daily oral doses of 15mg/kg. Oxybutynin
hydrochloride was not teratogenic in rats and rabbits at oral dose levels
(20mg/kg/day in rats and 48mg/kg/day in rabbits) which did not cause
significant maternal toxicity. At maternally toxic doses of oxybutynin
(100mg/kg/day), increased incidence of extra thoracolumbar ribs in rat foetuses,
as well as mortality of neonates, was observed. At oral daily dose levels up to
20mg/kg in rats, oxybutynin hydrochloride had no adverse effects on gestation
or on the birth and development of offspring up to weaning.

6.

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Lactose Monohydrate
Microcrystalline Cellulose
Calcium Stearate
Indigo Carmine (Aluminium Lake) E132

6.2

Incompatibilities
None known

6.3

Shelf life
3 years

6.4

Special precautions for storage
Store below 25°C in a dry place. Protect from light.

6.5

Nature and contents of container
Polypropylene tablet container with tamper-evident polyethylene cap.
Pack sizes: 20, 30, 50, 60, 84, 90, 100, 250, 500
PVC (250µm ± 5µm)/aluminium foil (20µm) blister packs.
Pack sizes: 20, 30, 50, 56, 60, 84, 90, 100
Not all pack sizes may be marketed.

6.6

Instructions for use and handling
No specific instructions for use/handling

7.

MARKETING AUTHORISATION HOLDER
Strides Pharma UK Ltd
Unit 4 Metro Centre
Tolpits Lane
Watford
Hertfordshire
WD18 9SS
Trading as: Co-pharma

8.

MARKETING AUTHORISATION NUMBER(S)
PL 13606/0070

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
21/03/2006

10

DATE OF REVISION OF THE TEXT
27/04/2017

Expand Transcript

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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